药物溶出仿生系统研究黄芩苷固体制剂的释放规律

中国临床药理学与治疗学 ›› 2010, Vol. 15 ›› Issue (1): 11-20.

药物溶出仿生系统研究黄芩苷固体制剂的释放规律

祝诚诚¹, 李自强¹, 刘志东^2,3,4, 高国义⁴, HAJI Juma¹, 舒乐欣⁴, 何新^1,2,3

¹天津中医药大学中药学院, ²教育部方剂学重点实验室, ³天津市中药化学与分析重点实验室, ⁴天津中医药大学中医药研究院, 天津300193

收稿日期:2009-09-30 修回日期:2009-12-23 出版日期:2010-01-26 发布日期:2020-09-21
通讯作者: 何新, 女, 教授, 博士生导师, 主要从事中药药代动力学研究。Tel: 022-23055511-2238 E-mail: hexintn@yahoo.com
作者简介:祝诚诚, 女, 硕士研究生在读, 研究方向: 中药学。Tel: 13821472983 E-mail: zhucheng_0829@163.com
基金资助:
国家重大新药创制专项(2009ZX09304-002); 国家自然科学基金项目(30772778); 国际科技合作计划项目(2007DFC31670); 天津市自然科学基金项目(07JCYBJC18800); 国家高等学校博士学科点专项科研基金项目(200800630005); 国家中医药管理局中医药行业科研专项(200807051)

Evaluation on the release discipline of baicalin and its three solid preparations using a drug dissolution simulating system

ZHU Cheng-cheng¹, LI Zi-qiang¹, LIU Zhi-dong^2,3,4, GAO Guo-yi⁴, HAJI Juma¹, SHU Le-xin⁴, HE Xin^1,2,3

¹College of Chinese Materia Medica, Tianjin University of Trad it ional Chinese Medicine; 2 Key Laboratory of Pharmacology of Traditional Chinese Medical Formulae (Tianjin University of Traditional Chinese Medicine) Ministry of Education; 3 Tianjin Key Laboratory of TCM Chemistry and Analysis; 4 Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China

Received:2009-09-30 Revised:2009-12-23 Online:2010-01-26 Published:2020-09-21

摘要/Abstract

摘要： 目的应用连续动态的药物溶出仿生系统(drug dissolution simulating system, DDSS) 研究黄芩苷原料药及其普通片、缓释片、固体脂质纳米粒冻干粉等三种固体制剂的体外释放特性, 为药物剂型设计研究提供新技术和新方法。方法分别采用连续动态的DDSS和桨法体外释放度实验, 对黄芩苷三种不同固体制剂进行体外释放度研究。以高效液相色谱法测定含量, 用SPSS 软件对数据进行模型拟合, 从拟合方程中提取T50 、Td 、m 等溶出参数, 并对两种溶出系统的释药规律进行相关性评价。结果黄芩苷普通片及其缓释片在两种溶出系统中释放特性分别都符合Weibull、Higuchi 方程。分别对黄芩苷普通片及其缓释片在两种溶出系统中释放结果进行相关性评价, 相关水平r 值各为0. 975 、0. 9995, 均大于临界值(r4, 0. 01 =0. 917), 即相关性良好。黄芩苷原料药和固体脂质纳米粒冻干粉在连续动态DDSS 的释放特性均符合Weibull方程。结论该DDSS 模拟了一个连续动态的、更接近人体消化道环境的释药过程, 其体外溶出度研究结果与《中华人民共和国药典》(2005 年版二部) 溶出度测定法(桨法) 的良好相关性表明该DDSS 作为评价药物固体制剂释药特性研究的合理性, 为药物剂型设计研究提供了新的技术平台。

关键词: 药物溶出仿生系统(DDSS), 桨法, 黄芩苷, 释放曲线

Abstract: AIM: To study the release features of the baicalin crude drug s and three baicalin so lid preparations such as ordinary tablets, sustained-release tablets and solid lipid nanoparticles by using a continuously dynamic drug dissolution simulating system (DDSS), and to provide a new technology and a new method for the study of devising drug preparations.METHODS: The DDSS method and the oar method were used to study their release features of three different baicalin solid preparations, respectively.Furthermore, the high performance liquid chromatography method was used to determine the contents of baicalin.The data were fitted by SPSS software, and the dissolution parameters such as T50, Td, m were extracted from the fittinge quations, and the correlation between the two systems were estimated.RESULTS: The release equations of the ordinary tablets and the sustained-release tablets of baicalin, in the two diffe rent systems, were Weibull and Higuchi equations, respectively.When the correlation of the release results of the baicalin tablets and the sustained-release tablets in the two different dissolution systems were evaluated, respectively, their corresponding correlational values were 0.975 and 0.9995, which were greater than the critical values (r4, 0.01 =0.917).It means they have a goo d correlation.The release features of the crude drug s and the solid lipid nanoparticles of baicalin on DDSS fit to Weibull equations. CONCLUSION: The DDSS simulates a drug release course which is continuously dynamic and close to the gastrointestinal tract environment. The release feature result s of DDSS and the oar methods embodied to Chinese Pharmacopoeia (edited in 2005) correlated well, which illustrated the reasonableness of the simulating systems to assess the release features of solid preparations.It provides a new technology plat form to the study of devising drug preparations.

Key words: Drug dissolution simulating system, Oar method, Baicalin, Release feature

中图分类号:

R969.1

祝诚诚, 李自强, 刘志东, 高国义, HAJI Juma, 舒乐欣, 何新. 药物溶出仿生系统研究黄芩苷固体制剂的释放规律[J]. 中国临床药理学与治疗学, 2010, 15(1): 11-20.

ZHU Cheng-cheng, LI Zi-qiang, LIU Zhi-dong, GAO Guo-yi, HAJI Juma, SHU Le-xin, HE Xin. Evaluation on the release discipline of baicalin and its three solid preparations using a drug dissolution simulating system[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2010, 15(1): 11-20.

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